Angiotensin-II-human-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEAngiotensinIIhumanCat.No.:HY-13948CASNo.:4474-91-3分?式:C??H??N??O??分?量:1046.18Sequence:Asp-Arg-Val-Tyr-Ile-His-Pro-PheSequenceDRVYIHPFShortening:作?靶點(diǎn):AngiotensinReceptor;Apoptosis作?通路:GPCR/GProtein;Apoptosis儲(chǔ)存?式:Protectfromlight,storedundernitrogenPowder-80°C2years-20°C1year*Insolvent:-80°C,6months;-20°C,1month(protectfromlight,storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:50mg/mL(47.79mM;Needultrasonic)掃描?維碼，DMSO:16.67mg/mL(15.93mM;Needultrasonic)運(yùn)?溶解?案計(jì)算器獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.9559mL4.7793mL9.5586mL5mM0.1912mL0.9559mL1.9117mL10mM0.0956mL0.4779mL0.9559mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1/3www.MedChemEwww.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥0.83mg/mL(0.79mM);Clearsolution此?案可獲得≥0.83mg/mL(0.79mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL8.3mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請(qǐng)依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥0.83mg/mL(0.79mM);Clearsolution此?案可獲得≥0.83mg/mL(0.79mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL8.3mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥0.83mg/mL(0.79mM);Clearsolution此?案可獲得≥0.83mg/mL(0.79mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。4.以1mL?作液為例，取100μL8.3mg/mL的澄請(qǐng)依序添加每種溶劑：PBSDMSO儲(chǔ)備液加到900μL??油中，混合均勻。Solubility:30mg/mL(28.68mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性AngiotensinIIhuman(AngiotensinII)主作?于AT1受體的?管收縮劑。AngiotensinIIhuman刺激交感神經(jīng)刺激，增加醛酮的?物合成和腎功能。AngiotensinIIhuman誘導(dǎo)?管平滑肌細(xì)胞的?長(zhǎng)，增加成纖維細(xì)胞中I型和III型膠原的合成，導(dǎo)致?管壁和?肌增以及纖維化。AngiotensinIIhuman還可誘導(dǎo)細(xì)胞凋亡(apoptosis)。IC50&TargetAngiotensinreceptor(ATreceptor)[1]體外研究MostoftheknownactionsofAngiotensinII(AngII)aremediatedbyAT1receptors,theAT2receptorcontributestotheregulationofbloodpressureandrenalfunction[1].AngiotensinIIraisesbloodpressure(BP)byanumberofactions,themostimportantonesbeingvasoconstriction,sympatheticnervousstimulation,increasedaldosteronebiosynthesisandrenalactions.OtherAngiotensinIIactionsincludeinductionofgrowth,cellmigration,andmitosisofvascularsmoothmusclecells,increasedsynthesisofcollagentypeIandIIIinfibroblasts,leadingtothickeningofthevascularwallandmyocardium,andfibrosis.Theseactionsaremediatedbytype1AngIIreceptors(AT1)[2].Atthecellularlevel,responsivenesstoAngiotensinIIisconferredbytheexpressionofthetwoclassesofangiotensinreceptors(AT1andAT2).TheeffectsofAngiotensinIItoincreasebloodpressurearemediatedbyAT1receptors[3].體內(nèi)研究TodistinguishtheAT1receptorpopulationthatiscriticalforthepathogenesisofhypertension,oeachanimaltoinfuseAngiotensinII(1,000ng/kg/min)continuouslyfor4weeks.AngiotensinIIcauseshypertensionbyactivatingAT1receptorsinthekidneypromotingsodiumreabsorption[3].PROTOCOL2/3www.MedChemEwww.MedChemEAnimalMice[3]Administration[3](129×C57BL/6)F1micelackingAT1AreceptorsforAngiotensinIIareused.Themicearefed10gm/daygelled0.25%NaCldietthatcontainsallnutrientsandwater.After1weekofbaselinecollections,theanimalsareimplantedwithosmoticminipumpsinfusingAngiotensinIIandarereturnedtothemetaboliccagefor5moredays.UrinarysodiumcontentisdeterminedbyusinganIL943AutomaticFlamephotometer.After28daysofAngiotensinIIinfusion,heartsareharvested,weighed,fixedinformalin,sectioned,andstainedwithMassontrichrome.Allofthetissuesareexaminedbyapathologist(P.R.)withoutknowledgeofgenotypes.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CircRes.2020Mar13;126(6):e15-e29.?JCIInsight.2020Jul9;5(13):e138505.?PharmacolRes.2020Dec19;164:105391.?OxidMedCellLongev.2019Nov23;2019:4025496.?ActaPharmacolSin.2020Oct28.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].deGasparoM,etal.Internationalunionofpharmacology.XXIII.TheangiotensinIIreceptors.PharmacolRev.2000Sep;52(3):415-72.[2].FyhrquistF,etal.RoleofangiotensinIIinbloodpressureregulationandinthepathophysiologyofcardiovasculardisorders.JHumHypertens.1995Nov;9Suppl5:S19-24.[3].CrowleySD,etal.AngiotensinIIcauseshypertensionandcardiachypertrophythroughitsreceptorsinthekidney.ProcNatlAcadSciUSA.2006Nov21;103(47):17985-90.McePdfHeight關(guān)注MCE中國(guó)公眾號(hào)，